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Edicotinib

Catalog No. T15199 CAS 1142363-52-7

Synonyms: JNJ-40346527, JNJ-527

Edicotinib is a brain penetrant and orally active inhibitor of the colony-stimulating factor-1 receptor (IC50: 3.2 nM). It shows less inhibitory effects on KIT and FLT3 (IC50: 20 nM and 190 nM). It has the potential for Alzheimer's disease and rheumatoid arthritis treatment.

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Edicotinib, CAS 1142363-52-7

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Purity: 98%

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Description	Edicotinib is a brain penetrant and orally active inhibitor of the colony-stimulating factor-1 receptor (IC50: 3.2 nM). It shows less inhibitory effects on KIT and FLT3 (IC50: 20 nM and 190 nM). It has the potential for Alzheimer's disease and rheumatoid arthritis treatment.
Targets&IC50	FLT3:190 nM, Kit:20 nM , CSF-1R:3.2 nM
In vitro	Edicotinib (0.1 nM-1μM; 24 hours) causes a dose-dependent decrease of CSF1R activation. Edicotinib (0.1 nM-1μM; 24 hours) lead to a concurrent reduction of ERK1 and ERK2 phosphorylation. The dose-response curve displays the effect of Edicotinib on CSF1R and ERK1/2 (IC50: 18.6 nM and 22.5 nM for CSF1R and ERK1/2) [1].
In vivo	Edicotinib (oral gavage; 30 mg/kg; 33 days) significantly reduces the density of microglia in CA1 of the hippocampus of ME7-prion mice (PU.1+ cells) by up to 30%. And the expression of IL-1β is also reduced, however not other inflammatory cytokines. Edicotinib (oral gavage; 3, 10, 30, and 100 mg/kg; 5 days) obviously inhibits microglial proliferation in ME7 mice.?It reduces the number of microglia (total CD45+CD11b+ cells) only at the highest dose tested of 100 mg/kg. At every dose tested (CD45+CD11b high Ly6C intermediate/low cells), JNJ-527 depletes up to 50% of patrolling blood monocytes. Only a tendency for a reduction in the proportion of inflammatory monocytes (Ly6C high?cells) at 100 mg/kg [1]. Edicotinib displays a good pharmacokinetic/pharmacodynamics (PK/PD) profile, the microglial proliferation data shows an EC50 of 196/ml and 69 ng/g calculated from plasmatic and brain compound concentration, respectively [1].

Synonyms	JNJ-40346527, JNJ-527
Molecular Weight	461.61
Formula	C27H35N5O2
CAS No.	1142363-52-7

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 15 mg/mL (32.4 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Mancuso R, et al. CSF1R inhibitor JNJ-40346527 attenuates microglial proliferation and neurodegeneration in P301S mice.Brain. 2019 Oct 1;142(10):3243-3264. 2. Genovese MC, et al. Results from a Phase IIA Parallel Group Study of JNJ-40346527, an Oral CSF-1R Inhibitor, in Patients with Active Rheumatoid Arthritis despite Disease-modifying Antirheumatic Drug Therapy.J Rheumatol. 2015 Oct;42(10):1752-60.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library Inhibitor Library Immunology/Inflammation Compound Library Anti-Alzheimer's Disease Compound Library Drug Repurposing Compound Library Kinase Inhibitor Library CNS-Penetrant Compound Library Angiogenesis related Compound Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library

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Keywords

Edicotinib 1142363-52-7 蛋白酪氨酸激酶血管生成 c-Fms c-Kit CSF-1R FLT colony stimulating factor 1 receptor CSF-1 receptor JNJ-527 JNJ527 inhibit JNJ40346527 neurodegeneration CSF1R JNJ 527 Inhibitor expansion alzheimer’s disease rheumatoid microglial JNJ 40346527 JNJ-40346527 arthritis inhibitor

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